期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 60, 期 20, 页码 8580-8590出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.7b01133
关键词
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Phosphonamidate 3a of methoxymethylphosphonic acid (MMPA) with propofol (l) and L-alanine ethyl ester was found to be an efficient scaffold for the oral delivery of compound 1. The synthesis and evaluation of MMPA based phosphonamidates of compound 1, HSK3486 (2), and other phenolic drugs revealed the general application of MMPA as the effective delivery vehicle for phenolic drugs. On the basis of plasma concentrations of compound 1 and SN38 (14), the oral bioavailability of compound 3a and 15 in beagle dogs was found to be 97.6% and 34.1%, respectively.
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